Preparation of rotamer mixtures of pharmaceutical salts

Details Preparation of rotamer mixtures of pharmaceutical salts Preparation of rotamer mixtures of pharmaceutical salts

2005-08-30

2005-08-30

Desai, Rita (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C546S190000

Reexamination Certificate

active

06936718

ABSTRACT:
In one embodiment, the present invention discloses a process to directly prepare an unequal ratio of specific, preferred rotamer or rotameric pair of an acid salt from a basic compound, by creative choice of a solvent medium. The process is particularly useful in preparing desired rotamers of pharmaceutically useful salts.

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patent: WO 00/66559 (2000-11-01), None
Salt Selection for basic drugs 1986, Philip Gould.
Ananda Palani et al Discovery of 4-[(Z)-](4-Bromo . . . Oct. 11, 2001.
Julie Strizki et al SCH- C (SCH 351125), . . . Oct. 2001.
Rizzo et al., “Equilibrium and Kinetics of Rotamer Interconversion in Immunosuppressant Prodigiosin Derivatives in Solution”,J. Pharmaceutical Sciences, Jan. 1999, 88(1):73-78.
Palani et al., “Discovery of 4-[(Z)-(4-Bromophenyl)-(ethoxyimino)methyl]-1′-[2,4-dimethyl-3-pyridinyl)carbonyl]-4′-methyl-1,4′-bipiperidine N-Oxide (SCH 351125): An Orally Bioavailable Human CCR5 Antagonist for the Treatment of HIV Infection”,J. Medical Chemistry, Oct. 11, 2001, 44(21): 3339-3342.
S. Berge et al., “Pharmaceutical Salts”,J. of Pharmaceutical Sciences, 66(1): 1-19 (1977).
P. Gould et al., “Salts Selection for Basic Drugs”,International J. of Pharmaceuticsl, 33:201-217 (1986).

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